Neurological Disease

Fasciculin-I is isolated from the mambas venom. Fasciculin-I exerts its toxic effects by inhibiting acetylcholinesterase (AChE). Fasciculin-I blocks α-neurotoxins of nicotinic acetylcholine receptors and cardiac toxins that interact with cell membranes .

AChE/BChE-IN-2 (Compound 13b) is a potent inhibitor of AChE/BChE (AChE IC50 = 0.96 ± 0.14 µM, BChE IC50 = 1.23 ± 0.23 µM). AChE/BChE-IN-2 has the potential for the research of AD diseases.

AVLX-125 (UCCB01-125) is a PSD-95 and PDZ domain inhibitor with K_d value of 10 nM. AVLX-125 can be used in the study of inflammatory pain.

Sacubitril (sodium) (Standard) is the analytical standard of Sacubitril (sodium). This product is intended for research and analytical applications. Sacubitril sodium is a potent and orally active NEP (neprilysin) inhibitor, with an IC50 of 5 nM. Sacubitril sodium enhances the tone of the natriuretic peptide (NP) system and exerts significant antihypertensive effects. Sacubitril sodium is a component of the heart failure medicine LCZ696. Sacubitril sodium can be used for the research of heart failure, hypertension and COVID-19.

GL-II-73 is a selective, orally active and blood-brain barrier permeable positive allosteric modulator of α5GABA_A receptor, acting on the benzodiazepine-binding site of GABA_A receptors. The binding selectivity of GL-II-73 for the α5 subtype is 6-, 11- and 12.5-fold higher than that for the α2, α1 and α3 subtypes, respectively. GL-II-73 reverses pilocarpine-induced hyperactivation of dopamine neurons in the ventral tegmental area, improves working memory and pyramidal neuron dendritic morphology in 5xFAD mice, but does not reduce β-amyloid load. GL-II-73 can be used in research related to Alzheimer's disease and temporal lobe epilepsy with comorbid psychosis.

Cholesterol 24-hydroxylase-IN-3 is an orally active, selective, and blood-brain barrier-penetrant CH24H inhibitor (IC₅₀ = 23 nM) belonging to 1,3-oxazole derivatives. Cholesterol 24-hydroxylase-IN-3 competitively inhibits CH24H enzyme activity by using the 1,3-oxazole nitrogen atom to coordinate the heme iron and the cyclopropyl group occupying the hydrophobic pocket. Cholesterol 24-hydroxylase-IN-3 can be used for research on epilepsy and other neurological diseases.

Tripelennamine is a histamine H1-receptor antagonist. Tripelennamine effectively reverses histamine-induced bronchoconstriction, increased transpulmonary pressure, elevated pulmonary vascular resistance and reduced dynamic compliance. Tripelennamine does not significantly affect arterial hypoxemia, hemoglobin desaturation and hypercapnia in horses undergoing short-term high-intensity exercise. Tripelennamine exhibits local and central analgesic activity. Tripelennamine can be used in studies related to emphysema, urticaria and acute laminitis.

Isoliquiritin (Standard) is the analytical standard of Isoliquiritin. This product is intended for research and analytical applications. Isoliquiritin, isolated from Licorice Root, inhibits angiogenesis and tube formation. Isoliquiritin also exhibits antidepressant-like, anti-oxidative, anti-Inflammatory effects and antifungal activity.

Org37684 is a highly potent 5-HT_2C receptor agonist (pEC₅₀=8.17). Org37684 exhibits a rank order of potency of 5-HT_2C>5-HT_2B>5-HT_2A. Its selectivity for the 5-HT2C receptor is approximately 2.5 times over the 5-HT2B (pEC₅₀=7.96) and ten times for the 5-HT_2A (pEC₅₀=7.11) receptor.

Neurofilament, U-¹⁵N is the ¹⁵N-labeled Neurofilament.

Amdakefalin is a μ and δ opioid receptors agonist with analgesic effects.

PF-06371900 is a potent and highly selective leucine rich repeat kinase 2 (LRRK2) inhibitor.

Antazoline (hydrochloride) (Standard) is the analytical standard of Antazoline (hydrochloride). This product is intended for research and analytical applications. Antazoline hydrochloride is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline hydrochloride can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline hydrochloride can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline hydrochloride can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC₅₀ of 2.910 μmol/L in HepAD38 cells. Antazoline hydrochloride also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC₅₀ = 2.349 μmol/L). Antazoline hydrochloride has anti-arrhythmic effect in acute myocardial infarctions. Antazoline hydrochloride can be studied in research for cardiovascular diseases, and HBV.

AP102 is a dual SSTR2/SSTR5-specific somatostatin analog (SSA). AP102 is a disulfide-bridged octapeptide SSA containing synthetic iodinated amino acids. AP102 binds with subnanomolar affinity to SSTR2 and SSTR5 (IC₅₀: 0.63 and 0.65 nM, respectively). AP102 does not bind to SSTR1 or SSTR3. AP102 can be used for acromegaly and neuroendocrine tumors research.

Nialamide hydrochloride is a non-selective monoamine oxidase (MAO) inhibitor. Nialamide hydrochloride inhibits MAO and regulates ROS production. Nialamide hydrochloride induces hyperkinesis in animals, enhances the anticonvulsant effect of Diphenylhydantoin in mice, increases rectal temperature, and enhances the pressor effect of Norepinephrine. Nialamide hydrochloride can be used in the research of depression, inflammatory diseases, neurodegenerative diseases, and hypertension.

4,5-DiHDPA lactone (5), a derivative of docosahexaenoic acid (DHA), is a PPARγ activator.

CP-465022 hydrochloride is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC₅₀ of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes.

GW559090 is a selective, competitive, and high-affinity α4 integrin antagonist with a K_d of 0.19 nM for α4β1. GW559090 can effectively block the binding of α4β1 to vascular cell adhesion molecule 1 (VCAM-1) and fibronectin with IC₅₀ values of 7.72 and 8.04 nM. GW559090 also inhibits the interaction between α4β7 and mucosal addressin cell adhesion molecule 1 (MAdCAM-1) (IC₅₀ = 23 nM). GW559090 can inhibit inflammatory infiltration in the eyes, repair the corneal barrier and restore the function of goblet cells. GW559090 can be used for research of Sjögren's syndrome associated dry eye.

sEH-IN-22 (Compound 1) is a soluble epoxide hydrolase (sEH) inhibitor (IC₅₀ = 1.1 μM) found in Rubia philippinensis. sEH-IN-22 exhibits anti-inflammatory, analgesic and blood pressure-regulating effects. sEH-IN-22 can be used for the researches of inflammation, neurological and cardiovascular disease.

α-Pyrrolidinocyclohexanophenone hydrochloride is a drug derivative.